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Drug Delivery

Qing Chang, Rui Geng, Shanzheng Wang, Ding Qu, Xiangfei Kong
Treatment for multiple myeloma (MM) with a combined strategy of bone and tumor targeting remains a crucial technical challenge due to the incorporation of various functional components into one single system. Here, we developed dioleoyl phosphatidic acid (DOPA)-based paclitaxel (PTX)-loaded liposomes with modifications of alendronate and transferrin (Ald-/Tf-modified PTX-L), which were capable of bone affinity mediated by phosphate groups in DOPA and alendronate, and tumor targeting offered by transferrin. Ald-/Tf-modified PTX-L had clear and well-defined spherical shape with an intermediated size of 118...
October 17, 2016: Drug Delivery
Shouwen Zhang, Jie Wang, Jin Pan
CONTEXT: Baicalin has many pharmacological activities, including protective function against myocardial ischemia by antioxidant effects and free radical scavenging activity. However, its rapid elimination half-life in plasma and poor water solubility limits its clinical efficacy. OBJECTIVE: Novel baicalin-loaded PEGylated nanostructured lipid carriers (BN-PEG-NLC) were developed to improve bioavailability of BN, to prolong retention time in vivo and to enhance its protective effect...
October 17, 2016: Drug Delivery
Hong Jiang, Dongming Geng, Hongqia Liu, Zhengrong Li, Jing Cao
CONTEXT: Gastric carcinoma (GC) is one of the most common cancers and the second most frequent cause of cancer-related deaths. Chemotherapy is an important therapeutic modality for GC. However, chemoresistance limited its success rate. Combination chemotherapy is often applied to prevent drug-induced resistance in cancers. OBJECTIVE: The aim of this study is to evaluate whether the co-delivery of etoposide (ETP) and curcumin (CUR) with one nanoparticle can result in synergistic effects of both drugs...
October 17, 2016: Drug Delivery
Arijit Guha, Nikhil Biswas, Kaustav Bhattacharjee, Nityananda Sahoo, Ketousetuo Kuotsu
OBJECTIVE: The objective of the present study was to develop novel PMV [poly (methacrylic acid-co-vinyl triethoxylsilane)]-coated mesoporous silica nanoparticles (MSN) with improved hypoglycemic effect for oral insulin (INS) delivery. METHODS: MSN was synthesized under acidic condition using Pluronic® P 123 and Tetra ethoxy orthosilane. Surfactant was removed by calcination. Calcined MSN was coated with pH sensitive polymer PMV. Cytotoxicity of this coated MSN was evaluated by MTT assay using CHO-K1 cell line...
October 17, 2016: Drug Delivery
Wenping Wang, Yaqin Cai, Guangxing Zhang, Yanhua Liu, Hong Sui, Kinam Park, Hong Wang
Lung-targeting sophoridine-loaded poly(lactide-co-glycolide) (PLGA) microspheres were constructed by a simple oil-in-oil emulsion-solvent evaporation method. The obtained microspheres were systematically studied on their morphology, size distribution, drug loading, encapsulation efficiency, in vitro release profile, and biodistribution in rats. The drug-loaded microparticles showed as tiny spheres under SEM and had an average size of 17 μm with 90% of the microspheres ranging from 12 to 24 μm. The drug loading and encapsulation efficiency were 65% and 6...
September 30, 2016: Drug Delivery
J T Sutton, K J Haworth, S K Shanmukhappa, M R Moody, M E Klegerman, J K Griffin, D M Patton, D D McPherson, C K Holland
Ultrasound is both a valuable diagnostic tool and a promoter of beneficial tissue bioeffects for the treatment of cardiovascular disease. Vascular effects can be mediated by mechanical oscillations of circulating microbubbles that may also encapsulate and shield therapeutic agents in the bloodstream. Here, the effect of color-Doppler ultrasound exposure on bevacizumab-loaded liposome delivery into the vascular bed was assessed in atheromatous porcine carotids. Bevacizumab, an anti-angiogenic antibody to vascular endothelial growth factor (VEGF-A), was loaded into echogenic liposomes (BEV-ELIP) and confirmed to be immunoreactive...
September 30, 2016: Drug Delivery
Nirav Patel, Happy Nakrani, Mihir Raval, Navin Sheth
A novel cationic nanoemulsified in-situ ophthalmic gel of loteprednol etabonate (LE) was developed to improve the permeability and retention time of formulations for overall improvement of drug's ocular bioavability. Capryol 90 (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) was selected as formulation excipients to construct pseudoternary phase diagrams and nanoemulsion region was recognized from diagrams. Spontaneous emulsification method was used to manufacture LE nanoemulsion and it was optimized using 3(2) factorial design by considering the amount of oil and the ratio of surfactant to cosurfactant (Smix) as independent variables and evaluated for various physicochemical properties...
September 30, 2016: Drug Delivery
Samia A Nour, Nevine S Abdelmalak, Marianne J Naguib, Hassan M Rashed, Ahmed B Ibrahim
Clonazepam (CZ) is an anti-epileptic drug used mainly in status epilepticus (SE). The drug belongs to Class II according to BCS classification with very limited solubility and high permeability and it suffers from extensive first-pass metabolism. The aim of the present study was to develop CZ-loaded polymeric micelles (PM) for direct brain delivery allowing immediate control of SE. PM were prepared via thin film hydration (TFH) technique adopting a central composite face-centered design (CCFD). The seventeen developed formulae were evaluated in terms of entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and in vitro release...
September 20, 2016: Drug Delivery
Hyosook Hwang, Hyeon-Soo Kim, Hwan-Seok Jeong, Bagalkot Tarique Rajasaheb, Minjoo Kim, Phil-Sun Oh, Seok Tae Lim, Myung-Hee Sohn, Hwan-Jeong Jeong
BACKGROUND: We investigated the therapeutic effectiveness of PEGylated liposomes loaded with angiogenic peptides for treating hindlimb ischemia. METHODS: Rats received a femoral artery occlusion. Red blood cells collected from the animals were labeled with technetium-99m. Limb perfusion gamma imaging was performed. PEGylated liposomes loaded with angiogenic peptides were administered intra-arterially. Technetium-99m red blood cell imaging was repeated 1 week later...
August 25, 2016: Drug Delivery
Bappaditya Chatterjee, Samah Hamed Almurisi, Ather Ahmed Mahdi Dukhan, Uttam Kumar Mandal, Pinaki Sengupta
Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug...
August 15, 2016: Drug Delivery
Yan Fang, Jianxiu Xue, Liyuan Ke, Yang Liu, Kai Shi
A kind of polymeric lipid vesicles (PLVs) with pH-responsive turning on-off membrane for programed delivery of insulin in gastrointestinal (GI) tract was developed, which was self-assembled from the grafted amphipathic polymer of N-tocopheryl-N'-succinyl-ɛ-poly-l-lysine (TP/SC-g-PLL). By controlling the grafting ratio of hydrophobic alkane and ionizable carboxyl branches, the permeability of membrane was adjustable and thus allowing insulin release in a GI-pH dependent manner. The effects of grafting degree of substitution (DS) on the pH-responsive behavior of the formed vesicles were confirmed by critical aggregation concentration determination, morphology and size characterization...
August 15, 2016: Drug Delivery
Hafsa Ahmad, Abhishek Arya, Satish Agrawal, Sheeba Saji Samuel, Sandeep Kumar Singh, Guru Raghavendra Valicherla, Neelam Sangwan, Kalyan Mitra, Jiaur R Gayen, Sarwesh Paliwal, Rakesh Shukla, Anil Kumar Dwivedi
Withania somnifera Dunal (Solanaceae) known as Ashwagandha, a popular plant of Indian origin is known to possess tremedous medicinal potential, often used as anti-inflammatory, anti-platelet, antihypertensive, hypoglycemic, hypolipidemic and adaptogenic candidate. Some of its chemotypes developed by CSIR, India includes NMITLI-101, NMITLI-118, NMITLI-128. In this study the investigators have attempted development of a phytosomal complex of NMITLI118RT + (standardized ethanolic extract of a new chemotype of W...
August 12, 2016: Drug Delivery
Mohammad Hemmati, Farhood Najafi, Reza Shirkoohi, Hamid Reza Moghimi, Amir Zarebkohan, Bahram Kazemi
hPAMAM/DNA polyplexes, compared to viral vectors, display unique characteristics including more safety, less immune response outcomes, a simpler synthesis and an easier process. Given the importance of these polymers, hPAMAM coated with the PEGDGA copolymer was developed as a promising non-viral gene carrier. In the present study, a new complex of hPAMAM, PEGDGA-modified hyperbranched polyamidoamine (hPAMAM), was established as a versatile non-viral gene vector. The hPAMAM polymer was synthesized by using a modified one-pot method...
August 5, 2016: Drug Delivery
Vikas Jhawat, Sumeet Gupta, Vipin Saini
In the present study, pluronic lecithin based organogels (PLO gels) were formulated as topical carrier for controlled delivery of mefenamic acid. Ten organogel formulations were prepared by a method employing lecithin as lipophilic phase and pluronic F-127 as hydrophilic phase in varying concentrations to study various parameters using in vitro diffusion study and in vivo studies. All formulations were found to be off-white, homogenous, and reluctant to be washed easily and have pH value within the range of 5...
August 5, 2016: Drug Delivery
Huipeng Li, Dongfen Yuan, Minjie Sun, Qineng Ping
Octreotide had been exploited as a targeting ligand for nanoparticle tumor localization over-expressing somatostatin receptor. In addition to particle size and other physiochemical properties, ligand density had great influence on the delivery of active targeted nanoparticles. Herein, octreotide targeted liposomal doxorubicin was constructed with different ligand density by post-inserting HSPE-PEG4000-Octreotide into pre-formed liposome. The octreotide ligand insertion was confirmed by activity detection of octreotide in HSPE-PEG4000-Octreotide with synchronous fluorescence...
July 18, 2016: Drug Delivery
Hongxia Cui, Peng Quan, Zhuang Zhou, Liang Fang
The aim of the study was to develop a drug-in-adhesive patch system for transdermal delivery of zaltoprofen (ZAL). The formulation was designed in combination with the ion pair and chemical enhancer strategy. Seven organic amines were chosen as counter ions, and the prepared ion pairs were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The in vivo pharmacokinetic performance of ZAL was studied on rabbits following transdermal and intravenous administration...
July 16, 2016: Drug Delivery
Shafi Ullah, Muhammad Raza Shah, Mohammad Shoaib, Muhammad Imran, Abdelbary M A Elhissi, Farid Ahmad, Imdad Ali, Syed Wadood Ali Shah
CONTEXT: Nonionic surfactant vesicles have gained increasing scientific attention for hydrophobic drugs delivery due to their biocompatibility, stability and low cost. OBJECTIVE: The aim of the present study was to synthesize and evaluate a novel creatinine-based nonionic surfactant in terms of its ability to generate biocompatible niosomal system for the delivery of Clarithromycin. MATERIALS AND METHODS: The surfactant was synthesized by reacting creatinine with lauroyl chloride followed by characterization using (1)HNMR and MS...
July 16, 2016: Drug Delivery
Juber Akhtar, Hefazat Hussain Siddiqui, Sheeba Fareed, Badruddeen, Mohammad Khalid, Mohammed Aqil
Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic β-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method...
July 2016: Drug Delivery
Li Zhang, Zhenqiu Gao, Xiuyun Zhao, Gaofu Qi
Surfactin, a natural lipopeptide produced by Bacillus, is gaining attention for potentially biomedical and pharmaceutical applications. Here, surfactin was assayed for oral delivery of insulin (INS) by its ability to bind to and promote protein to penetrate through the cell membrane. Analysis by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, surfactin was found to form co-precipitates with INS to protect it from acidic and enzymatic attack in the gastrointestinal tract. Further analysis by non-reductive electrophoresis showed surfactin could bind to INS forming heteropolymers...
July 2016: Drug Delivery
Ožbej Zupančič, Gintare Leonaviciute, Hung Thanh Lam, Alexandra Partenhauser, Snežana Podričnik, Andreas Bernkop-Schnürch
CONTEXT: Self-emulsifying drug delivery systems (SEDDS) are among most promising tools for improving oral peptide bioavailability. OBJECTIVE: In this study, in vitro protective effect of SEDDS containing desmopressin against presystemic inactivation by glutathione and α-chymotrypsin was evaluated. MATERIALS AND METHODS: The partitioning coefficient (log P) of desmopressin was increased via hydrophobic ion pairing using anionic surfactants...
July 2016: Drug Delivery
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